Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents.

Antitubercular Agents / chemical synthesis Dose-Response Relationship, Drug Drug Design Humans Microbial Sensitivity Tests Molecular Structure Mycobacterium tuberculosis / drug effects Nitrofurans / chemistry Oxadiazoles / chemistry Structure-Activity Relationship
Antitubercular activity Nitrofuran-1,3,4-oxadiazole hybrids Synthesis

Journal

Bioorganic & medicinal chemistry
ISSN: 1464-3391
Titre abrégé: Bioorg Med Chem
Pays: England
ID NLM: 9413298

Informations de publication

Date de publication:
01 01 2022
Historique:
received: 25 05 2021
revised: 30 09 2021
accepted: 19 11 2021
pubmed: 4 12 2021
medline: 24 2 2022
entrez: 3 12 2021
Statut: ppublish

Résumé

Three series of novel nitrofuran-1,3,4-oxadiazole hybrids were designed and synthesized as new anti-TB agents. The structure activity relationship study indicated that the linkers and the substituents on the oxadiazole moiety greatly influence the activity, and the substituted benzenes are more favoured than the cycloalkyl or heterocyclic groups. Besides, the optimal compound in series 2 was active against both MTB H

Identifiants

DOI: 10.1016/j.bmc.2021.116529 PMID: 34861474
pubmed: 34861474
pii: S0968-0896(21)00537-X
doi: 10.1016/j.bmc.2021.116529
pii:
doi:

Substances chimiques

Antitubercular Agents 0
Nitrofurans 0
Oxadiazoles 0
1,3,4-oxadiazole 20O2F20OUR

Types de publication

Journal Article Research Support, Non-U.S. Gov't

Langues

eng

Sous-ensembles de citation

IM

Pagination

116529

Informations de copyright

Copyright © 2021 Elsevier Ltd. All rights reserved.

Auteurs

Apeng Wang (A)

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Shijie Xu (S)

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Yun Chai (Y)

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; Institute of Medical Research, Northwestern Polytechnical University, 127 West Youyi Road, Xi'an 710072, China.

Guimin Xia (G)

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. Electronic address: xiaguimin@126.com.

Bin Wang (B)

Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital College of Pharmacy, Medical University, Beijing 100149, China.

Kai Lv (K)

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Dan Wang (D)

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Xiaoyu Qin (X)

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Bin Jiang (B)

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; Hebei Medical University, Shijiazhuang 050017, China.

Wenhao Wu (W)

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; Hebei Medical University, Shijiazhuang 050017, China.

Mingliang Liu (M)

Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. Electronic address: lmllyx@126.com.

Yu Lu (Y)

Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital College of Pharmacy, Medical University, Beijing 100149, China. Electronic address: luyu4876@hotmail.com.

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Classifications MeSH

questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antibactériens › Antituberculeux › Design, synthesis and biological evaluation of...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › Design, synthesis and biological evaluation of...
questionsmedicales.fr › Techniques d'investigation › Développement de médicament › Découverte de médicament › Conception de médicament › Design, synthesis and biological evaluation of...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Hominidae › Humains › Design, synthesis and biological evaluation of...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité microbienne › Design, synthesis and biological evaluation of...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › Design, synthesis and biological evaluation of...
questionsmedicales.fr › Bactéries › Bactéries à Gram positif › Bâtonnets à Gram positif › Bâtonnets asporogènes à Gram positif › Bâtonnets asporogènes réguliers à Gram positif › Mycobacteriaceae › Mycobacterium › Mycobacterium tuberculosis › Design, synthesis and biological evaluation of...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Furanes › Nitrofuranes › Design, synthesis and biological evaluation of...
questionsmedicales.fr › Composés hétérocycliques › Composés hétéromonocycliques › Azoles › Oxazoles › Oxadiazoles › Design, synthesis and biological evaluation of...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Design, synthesis and biological evaluation of...